The synthetic method of p-thymphenyl phenyl serine ethyl ester and p-thymphenyl phenyl serine ethyl ester

Abstract

The invention discloses a synthetic method of P-methyl sulfone phenyl ethyl serinate, comprising the steps of S1, adding ethyl glycinate hydrochloride into methanol, and heating to dissolve to form afirst solution; S2, adding copper sulfate pentahydrate in the first solution to form a second solution by dissolving; S3, adjusting PH value of the second solution to meet the condition for alkaline reaction, adding P-methylsufonyl benzaldehyde to allow reaction, and holding the temperature and controlling the PH value to keep reaction condition values during reaction; S4, recycling methanol in the reacted materials, adding water to the residue to form a third solution, cooling, and centrifugally separating to obtain P-methyl sulfone phenyl ethyl serinate. The ethyl glycinate hydrochloride andP-methylsufonyl benzaldehyde are subjected to further reaction under the catalytic action of copper sulfate and an organic base to generate a target product; no sulfuric acid is used in the reactionprocess, the amount of waste acid in waste water is decreased, and the environment is protected; dangers that may occur during sulfuric acid transport and production are avoided, better safety is provided, and operating efficiency can be improved.

Description

technical field [0001] The invention relates to a florfenicol intermediate and a synthesis method thereof, in particular to a synthesis method of p-thiamphenylphenylserine ethyl ester with high yield, less waste water and environmental protection and p-thiamphenylphenylserine ethyl ester ester. Background technique [0002] Florfenicol, also known as fluprofen and fluthiamphenicol, is a white or off-white crystalline powder, odorless, and bitter in taste. It is a new type of chloramphenicol for veterinary medicine that was successfully developed in the late 1980s. A class of broad-spectrum antibacterial drugs, which produce broad-spectrum antibacterial effects by inhibiting the activity of peptidyltransferases, and have a broad antibacterial spectrum, including various Gram-positive and negative bacteria and mycoplasma. [0003] It was first launched in Japan in 1990. In 1993, Norway approved the drug to treat salmon furunculosis. In 1995, France, the United Kingdom, Austri...

AI Technical Summary

Problems solved by technology

[0008] The above three methods all use a large amount of sulfuric acid for catalytic esterification, and a large amount of waste acid is produced during production, which is not conducive to environmental protection; , all need to be very cautious, so as not to cause harm to personnel and equipment, which is not conducive to increasing production rate

[0009] In addition, the above-mentioned method often needs to use p-thiamphenicyl benzaldehyde as the starting material, react with copper sulfate and glycine to generate copper p-thymphenyl phenylserine, and then react with absolute ethanol under the catalysis of concentrated sulfuric acid. After a series of To obtain p-thymphenylphenylserine ethyl ester, two steps are required, and the process is relatively cumbersome

[0010] At the same time, ethanol and sulfuric acid react to form water when heated, which is not conducive to the forward progress of esterification

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